tailieunhanh - Synthesis and bioactivities of 1-(4-hydroxyphenyl)-2-((heteroaryl)thio)ethanones as carbonic anhydrase I, II and acetylcholinesterase inhibitors

The discovery of enzyme targeting inhibitors is a popular area of drug research. Biological activities of the compounds bearing phenol and heteroaryl groups make them popular groups in drug design targeting important enzymes such as acetylcholinesterase (AChE, ) and carbonic anhydrases (CAs, EC ). The compounds 2 and 4 were found potent AChE inhibitors with the Ki values of ± nM and ± nM, respectively, while the compounds 2 (Ki = ± nM, on hCA I) and 1 (Ki = ± nM, on hCA II) had considerable CAs inhibitory potency. The lead compounds may help the scientists for the rational designing of an innovative class of drug candidates targeting enzyme-based diseases. |

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